Zolpidem-based orodispersible pharmaceutical tablet

a technology of orodispersible pharmaceutical tablets and zolpidem, which is applied in the directions of drug compositions, aerosol delivery, inorganic non-active ingredients, etc., can solve the problems of large variability between individuals, development of any new formulation comprising zolpidem is particularly problematic, and the development of a formulation which makes it possible both rapid disintegration and easy detection of misus

Inactive Publication Date: 2013-10-24
SANOFI SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0035]The tablet according to the invention is particularly advantageous since it makes it possible to reveal its antimisuse properties when it is introduced into a drink but not to reveal them in the mouth.
[0036]The tablet according to the invention also exhibits the advantage of having a release and an action of the active principle which are not detrimentally affected by the orodispersible formulation and the presence of components intended to be revealed during a possible misuse.

Problems solved by technology

However, there exists great variability between individuals in the bioavailability of a conventional immediate release formulation based on zolpidem.
Thus, development of any new formulation comprising zolpidem is particularly problematic, it being necessary for the pharmacokinetic and pharmacodynamic data not to vary unacceptably with respect to the results previously obtained for the conventional formulations, such as for the immediate release formulations sold by the Applicant Company under the trade names Ambien®, Stilnox® and Myslee®.
In addition, due to its hypnotic action, zolpidem might form the object of an abuse of use or of misuse.
The development of a formulation which makes possible both rapid disintegration and easy detection when misused is particularly complex in so far as the components introduced to counteract misuse can conflict with rapid disintegration of the said formulation.

Method used

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  • Zolpidem-based orodispersible pharmaceutical tablet
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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0103]Orodispersible Zolpidem Tartrate Tablets, Dosage 10 mg

[0104]Manufacturing Process (see FIGS. 1 and 2):

[0105]Zolpidem tartrate is mixed with anhydrous colloidal silica in a fluidized bed. The mixture is subsequently granulated in a fluidized bed using a suspension of amino-methacrylate copolymer. This suspension is preprepared by dispersing amino-methacrylate copolymer, sodium lauryl sulfate, stearic acid and hydrated colloidal silica in purified water, according to the recommendations of the supplier of amino-methacrylate copolymer.

TABLE 1UnitPercentageformulaformulaComposition(mg)(%)Zolpidem tartrate10.004.00Anhydrous colloidal silica (Aerosil ® 200, sold by0.200.08Evonik Degussa GmbH ®)Amino-methacrylate copolymer (Eudragit ® EPO,13.905.56sold by Evonik Degussa GmbH ®)Sodium lauryl sulfate (sold by Cognis ®)1.380.55Stearic acid (Stearic Acid 2236 ®, sold by2.060.83Mallinckrodt Baker ®)Hydrated colloidal silica (Syloïd ® FP 244, sold by4.821.93GRACE Davison ®)Mannitol (Pearli...

example 2

[0115]Orodispersible Zolpidem Tartrate Tablets, Dosage 5 mg

[0116]The orodispersible zolpidem tartrate tablets, dosed at 5 mg, are manufactured according to the same manufacturing process as that described in Example 1.

[0117]The composition is described in detail in the following Table 3.

TABLE 3Unit formulaPercentageComposition(mg)formula (%)Zolpidem tartrate5.002.50Anhydrous colloidal silica (Aerosil ® 200,0.100.05sold by Evonik Degussa GmbH ®)Amino-methacrylate copolymer (Eudragit ®6.933.47EPO, sold by Evonik Degussa GmbH ®)Sodium lauryl sulfate (sold by Cognis ®)0.680.34Stearic acid (Stearic Acid 2236 ®, sold by1.030.51Mallinckrodt Baker ®)Hydrated colloidal silica (Syloïd ® FP 244,2.401.20sold by GRACE Davison ®)Mannitol (Pearlitol ® 160C, sold by71.8635.92Roquette ®, and / or Parteck M200, sold byMerck ®)Crosslinked polyvinylpyrrolidone20.0010.00(Kollidon ® CL, sold by ISP ®)Aspartame (sold by Ajinomoto sweeteners3.001.50Europe SAS)Sodium stearyl fumarate (Pruv ®, sold by3.001.50J...

example 3

[0119]Orodispersible Zolpidem Tartrate Tablets, Dosage 2.5 mg

[0120]The orodispersible zolpidem tartrate tablets, dosed at 2.5 mg, are manufactured according to the same manufacturing process as that described in Example 1.

[0121]The composition is described in detail in the following Table 4.

TABLE 4Unit formulaPercentageComposition(mg)formula (%)Zolpidem tartrate2.501.67Anhydrous colloidal silica (Aerosil ® 200,0.050.03sold by Evonik Degussa GmbH ®)Amino-methacrylate copolymer(Eudragit ®3.472.32EPO, sold by Evonik Degussa GmbH ®)Sodium lauryl sulphate (sold by Cognis ®)0.340.23Stearic acid (Stearic Acid 2236 ®, sold by0.520.34Mallinckrodt Baker ®)Hydrated colloidal silica (Syloïd ® FP 244,1.200.80sold by GRACE Davison ®)Mannitol (Pearlitol ® 160C, sold by50.4033.6Roquette ®, and / or Parteck M200, sold byMerck ®)Crosslinked polyvinylpyrrolidone15.0010.00(Kollidon ® CL, sold by ISP ®)Aspartame (sold by Ajinomoto sweeteners2.251.50Europe SAS)Sodium stearyl fumarate (Pruv ®, sold by2.251....

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Abstract

The present invention is directed to oral pharmaceutical forms for rapid disintegration which make it possible to prevent possible misuse of the zolpidem present therein. The present invention thus relates to a zolpidem-based orodispersible tablet formulation intended to prevent abuse of use of the tablet at the expense of a third party.

Description

FIELD OF THE INVENTION[0001]The invention relates to a zolpidem-based orodispersible pharmaceutical tablet formulation intended to prevent possible abuse of use of the tablet at the expense of a third party. It also relates to a process for the preparation of the said tablet and to the use thereof.BACKGROUND OF THE INVENTION[0002]Zolpidem is a hypnotic active principle of the imidazopyridine category. It is generally administered orally in the form of tablets or in other solid forms. Zolpidem acts rapidly. The pharmacokinetic and pharmacodynamic data show that zolpidem has a rapid absorption and a rapid triggering of the hypnotic action. Its bioavailability is 70% following oral administration and exhibits linear kinetics in therapeutic doses lying between 5 and 10 mg according to conventional formulations, the plasma concentration peak is reached between approximately 0.5 and 3 hours, and the elimination half-life is short, with a mean of 2.4 hours and a duration of action of up to...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K47/02A61K9/20
CPCA61K47/02A61K9/2009A61K9/0007A61K31/437A61K33/10A61K9/0056A61K9/2081A61K9/5026A61P25/00A61P25/20
Inventor MARTINEZ, ANNICKROUGEOT, OLIVIERYAGUCHI, YOSHIKATSU
Owner SANOFI SA
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